Bioactivity | CMS-121 is a quinolone derivative and an orally active acetyl-CoA carboxylase 1 (ACC1) inhibitor. CMS-121 protects HT22 cells against ischemia and oxidative damage with EC50 values of 7 nM and 200 nM, respectively. CMS-121 has strong neuroprotective, anti-inflammatory, antioxidative and renoprotective activities[1][2][3]. | ||||||||||||
Target | Acetyl-CoA carboxylase 1 (ACC1) | ||||||||||||
Invitro | CMS-121 (1 µM; 4 hours; HT22 cells) treatment increases the phosphorylation of ACC1 at serine 79. CMS-121 can increase acetyl-CoA in cells[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
In Vivo | CMS-121 (~20 mg/kg; oral administration; daily; for 4 months; female SAMP8 mice) treatment reduces cognitive decline as well as metabolic and transcriptional markers of aging in the brain when administered to rapidly aging SAMP8 mice. CMS-121 preserves mitochondrial homeostasis by regulating acetyl-coenzyme A (acetyl-CoA) metabolism[1]. Animal Model: | ||||||||||||
Name | CMS-121 | ||||||||||||
CAS | 1353224-53-9 | ||||||||||||
Formula | C20H19NO3 | ||||||||||||
Molar Mass | 321.37 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Currais A, et al. Elevating acetyl-CoA levels reduces aspects of brain aging. Elife. 2019 Nov 19;8. pii: e47866. [2]. Chiruta C, et al. Chemical modification of the multitarget neuroprotective compound fisetin. J Med Chem. 2012 Jan 12;55(1):378-89. [3]. Prior M, et al. Back to the future with phenotypic screening. ACS Chem Neurosci. 2014 Jul 16;5(7):503-13. |